Investigational Drug Details
| Drug ID: | D085 |
| Drug Name: | Colesevelam |
| Synonyms: | Colesevelam |
| Type: | Chemical drug |
| DrugBank ID: | DB00930 |
| DrugBank Description: | Colesevelam is a bile acid sequestrant. Colesevelam is used with exercise and diet changes (restriction of cholesterol and fat intake) to reduce the amount of cholesterol and certain fatty substances in the blood. It works by binding bile acids in the intestine. Bile acids are made when cholesterol is broken down in the body. Removing these bile acids helps to lower blood cholesterol. |
| PubChem ID: | 56843207 |
| CasNo: | 182815-43-6 |
| Repositioning for NAFLD: | Yes |
| SMILES: | C(CCCCNCC=C)C[N+](C)(C)C.C(CCCNCC=C)CCCCCC.C(=C)CN.C(Cl)C1CO1.[Cl-] |
| Structure: |
|
| InChiKey: | NXOLVMFMAFCDSR-UHFFFAOYSA-M |
| Molecular Weight: | 581.802 |
| DrugBank Targets: | Bile acids binder |
| DrugBank MoA: | Colesevelam binds bile acids in the intestine and prevents their reabsorption. Colesevelam is not absorbed itself. The depletion of bile acid causes the upregulation of cholesterol 7-alpha-hydroxylase and conversion of cholesterol to bile acid. this increases the production and activity of hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase in the liver as well as an increase in the number of low density lipoprotein (LDL) receptors. This process clears LDL cholesterol from the blood. Serum triglyceride levels may increase or remain unchanged. The end result is increased clearance of LDL-cholesterol from the blood with decreased serum LDL-cholesterol. |
| DrugBank Pharmacology: | Colesevelam is a high capacity bile-acid binding molecule. Colesevelam binds to bile acids in the intestine which reduces the amount of bile acids that are returned to the liver via enterohepatic circulation. Clinical studies have demonstrated that elevated levels of total cholesterol (total-C), LDL-C, and apolipoprotein B (Apo B, a protein associated with LDL-C) are associated with an increased risk of atherosclerosis in humans. Similarly, decreased levels of high-density lipoprotein cholesterol (HDL-C) are associated with the development of atherosclerosis. Epidemiological investigations have established that cardiovascular morbidity and mortality vary directly with the levels of total-C and LDL-C, and inversely with the level of HDL-C. The combination of colesevelam and an HMG-CoA reductase inhibitor is effective in further lowering serum total-C and LDL-C levels beyond that achieved by either agent alone. |
| DrugBank Indication: | For use, alone or in combination with an HMG-CoA reductase inhibitor, as adjunctive therapy to diet and exercise for the reduction of elevated LDL cholesterol in patients with primary hypercholesterolemia (Fredrickson Type IIa). |
| Targets: | -- |
| Therapeutic Category: | Anticholesteremic drug |
| Clinical Trial Progress: | Phase 2 completed (NCT01066364) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0202 | NCT01066364 | Phase 2 | Completed | Has Results | February 2010 | July 21, 2020 | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00455 | 35075592 | Hepatol Int | Colesevelam ameliorates non-alcoholic steatohepatitis and obesity in mice. | Details |
| A21398 | 25349644 | World J Hepatol | Lipid-lowering agents in the management of nonalcoholic fatty liver disease. | Details |
| A21834 | 25015398 | Abdom Imaging | Cross-sectional and longitudinal evaluation of liver volume and total liver fat burden in adults with nonalcoholic steatohepatitis. | Details |
| A24275 | 23057494 | Aliment Pharmacol Ther | Review article: the emerging interplay among the gastrointestinal tract, bile acids and incretins in the pathogenesis of diabetes and non-alcoholic fatty liver disease. | Details |
| A24655 | 25755424 | J Clin Exp Hepatol | Management of Non-alcoholic Fatty Liver Disease and Steatohepatitis. | Details |
| A24854 | 22431131 | Hepatology | Effect of colesevelam on liver fat quantified by magnetic resonance in nonalcoholic steatohepatitis: a randomized controlled trial. | Details |
| A46922 | 34198609 | Cells | Colesevelam Reduces Ethanol-Induced Liver Steatosis in Humanized Gnotobiotic Mice. | Details |